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[]2005210218[](39800185);(30572248)3:,;:;Tel:024223986412;E2mail:guoliang222@gmail.com3,,(,110016)[],,,,[];;;;[]O625.3[]A[]1001-5094(2006)04-0145-06AdvancesintheResearchofResveratrolDerivativesandAnaloguesCHENGuo2liang3,GENGChun2mei,LIUXiang2yong(SchoolofPharmaceuticalEngineering,ShenyangPharmaceuticalUniversity,Shenyang110016,China)[Abstract]Thebiologicalandpharmaceuticalactivitiesandthestructure2activityrelationshipsofresveratrolderivativesandanalogswhichincludinghydroxyl,methyl,esterderivativesandsoonwerereviewedclassified2ly.Thesecompoundshavesomultiplebiologicalandpharmacologicalactivitiesasresveratrol,ofwhichsomearesuperiorinactivity,selectivityandstabilitytoresveratrolandhavebecomeafocusofresearchinrecentyears.[Keywords]Resveratrol;Derivative;Analog;Pharmacologicalactivity;Structure2activityrelationship1939,(1),80,,,(),1997Jang,1998,TPA(phorboldiester,,21222132)13,,2006,Vol.30,No.4145ProgressinPharmaceuticalSciences2006304145,piceatannol(2),,3,H+2K+2ATP,P450CYP1B1,piceatannol,[1]Murias[2],piceatannol,COX22,COX21IC5041713mol/L,COX22IC50010113mol/L,417108;4,3,52(3,4,5,3,4,52,3)COX21IC5001748mol/L,COX22IC500100104mol/L,719123;(celecoxib)COX21IC50191026mol/L,COX22IC500103482mol/L,546141,4,3,52,32COX22,42(3,4,5,42,4),,10mol/L40WI38VA,WI38;,42WI38VA,WI38[3]Murias[4](),32424,3,52(IC50216941155102mol/L),HL2603Sala[5],32PC3,Hung[6],32(LDL),32DPPH(1,12222),IC20711413mol/L;32160;,3210mol/L,32Stojanovic[7],42,3,52,43,5223,,,,,3,5,42(5),(IC504mol/L),;Caco22,013mol/L80%,014mol/L100%,(6)100[8];,30100,,[9]Cardile[10]27,2918,,,,,(GI50)2192mol/L,GI5024109mol/L,33,42(7)(GI5020063041461462006,Vol.30,No.4ProgressinPharmaceuticalSciences12124mol/L),3,4,42(8,GI5025139mol/L),,,,,,,Mor2ris[11]LNCaPDU145,,LNCaP,;Stivala[12],4Gosslau[13]424,3,4,5,42(MR24,9),,WI38VAIMR290SVHeLaLNCaPHT229HepG2,,WI38IMR290BJ2T,WI38VAIC50015mol/L,WI38IC5050mol/L,MR24[14],MR24HCA27HT229IC50626mol/L,,,Apc,012%MR24,227%24%,COX22[15]Matsuda[16],piceatannol3,5,42RBL22H32IC50211mol/L,IC50511mol/L,,,;,;piceatannol3,5,42(ionomycin)2TNF2IL243,523,52242(pterostilbene,,10),,COX21COX22(IC501918mol/L8319mol/L)HL260(IC50=70mol/L)DMBA()(ED50=418mol/L)(streptozotocen)(5)[17220],,22DNA40DNA,222DNA(aphidicolin)[21]B16M2F10,40mol/L60,,56%[22]Tolomeo[23],32BCR2ABL,,3,52Kerem[24]Rumexbu2cephalophorus5,42232(11)3,52242(12)Nam[25],3,5,2,42(13),,IC50018g/L,1817g/LLee[26],3,5,2,42,3,4,52242[27]A35,B,2006,Vol.30,No.4147ProgressinPharmaceuticalSciences2006304147TPA,3,5223,42(14)(32185%),(30123%),Ali[28](),,,(E)232252(15),(MLC)30mol/L,3[29](16),,Cardile[10]24226,2910(17),,452((E)2(42))21,32(DPK2DTSM202,18)B(nuclearfactorB,NFB)Kim[30]18P450s,P450s,B19Cardile[10]24,29,3,5,423,5,423,5,42,DU2145DeMedina[31]3,3,5,42(PDM2,20)(arylhydrocarbonreceptor,AhR)(Ki=112nmol/L),,,232O22D2242O22D2,,5,,,,20063041481482006,Vol.30,No.4ProgressinPharmaceuticalSciences[][1]PotterGA,Patterson1LH,Wanogho1E,etal.Thecancerpreventativeagentresveratrolisconvertedtotheanticancera2gentpiceatannolbythecytochromeP450enzymeCYP1B1[J].BrJCancer,2002,86(5):77427781[2]MuriasM,HandlerN,ErkerT,etal.Resveratrolanaloguesasselectivecyclooxygenase22inhibitors:synthesisandstruc2ture2activityrelationship[J].BioorgMedChem,2004,12(21):5571255781[3]LuJB,HoCT,GhaiG,etal.Resveratrolanalog,3,4,5,42tetrahydroxystilbene,differentiallyinducespro2apoptoticp53/Baxgeneexpressionandinhibitsthegrowthoftransformedcellsbutnottheirnormalcounterparts[J].Car2cinogenesis,2001,22(2):32123281[4]MuriasM,JagerW,HandlerN,etal.Antioxidant,prooxidantandcytotoxicactivityofhydroxylatedresveratrolanalogues:structure2activityrelationship[J].BiochemPhar2macol,2005,69(6):90329121[5]SalaG,MinutoloF,MacchiaM,etal.Resveratrolstructureandceramide2associatedgrowthinhibitioninprostatecancercells[J].DrugsExpClinRes,2003,29(526):26322691[6]HungLM,SuMJ,ChuWK,etal.Theprotectiveeffectofresveratrolsonischaemia2reperfusioninjuriesofratheartsiscorrelatedwithantioxidantefficacy[J].BrJPharmacol,2002,135(7):1627216331[7]StojanovicS,SprinzH,BredeO.Efficiencyandmechanismoftheantioxidantactionoftrans2resveratrolanditsanaloguesintheradicalliposomeoxidation[J].ArchBiochemBiophys,2001,391(1):792891[8]SchneiderY,ChabertP,StutzmannJ,etal.Resveratrolanalog(Z)23,5,42trimethoxystilbeneisapotentanti2mitoticdruginhibitingtubulinpolymerization[J].IntJCancer,2003,107(2):18921961[9]BelleriM,RibattiD,NicoliS,etal.Antiangiogenicandvascular2targetingactivityofthemicrotubule2destabilizingtrans2resveratrolderivative3,5,42trimethoxystilbene[J].MolPharmacol,2005,67(5):1451214591[10]CardileV,LombardoL,SpataforaC,etal.Chemo2enzymaticsynthesisandcell2growthinhibitionactivityofresveratrolanalogues[J].BioorgChem,2005,33(1):222331[11]MorrisGZ,WilliamsRL,ElliottMS,etal.ResveratrolinducesapoptosisinLNCaPcellsandrequireshydroxylgroupstodecreaseviabilityinLNCaPandDU145cells[J].Prostate,2002,52(4):31923291[12]StivalaLA,SavioM,CarafoliF,etal.Specificstructuraldeterminantsareresponsiblefortheantioxidantactivityandthecellcycleeffectsofresveratrol[J].JBiolChem,2001,276(25):225862225941[13]GosslauA,ChenM,H